Microwave-Assisted Multicomponent Syntheses of Heterocyclic Phosphonates

E. Bálint, Nóra Popovics-Tóth, Ádám Tajti, Bettina Rávai, K. Szabó, F. Perdih
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Abstract

Organophosphorus compounds play an important role in the medicinal- or agricultural industry, and in the human body as well. Over the last years, heterocyclic phosphonates have received growing interest due to their potential biological activity. An efficient tool for the preparation of such derivatives is their synthesis via multicomponent reactions. These transformations possess several criteria of an “ideal synthesis”, such as high atom economy, fast and simple accomplishment, energy efficiency, and environmentally friendliness. A number of heterocyclic phosphonates were prepared by us utilizing multicomponent syntheses. In this proceeding, the synthesis of the diethyl (2-amino-3-cyano-4H-chromen-4-yl)phosphonate by the condensation of salicylaldehyde, malononitrile and diethyl phosphite is briefly introduced. The reaction was optimized in respect of the catalyst type, the catalyst amount, the reaction time, and the temperature.
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微波辅助多组分合成杂环膦酸盐
有机磷化合物在医药或农业工业以及人体中发挥着重要作用。近年来,由于其潜在的生物活性,杂环膦酸盐受到越来越多的关注。制备此类衍生物的有效手段是通过多组分反应进行合成。这些转化具有“理想合成”的几个标准,如高原子经济性、快速简单的完成、能源效率和环境友好性。利用多组分合成技术制备了多种杂环膦酸盐。本文简要介绍了水杨醛、丙二腈和亚磷酸二乙酯缩合合成膦酸二乙酯(2-氨基-3-氰基-4-铬-4-基)。从催化剂类型、催化剂用量、反应时间、反应温度等方面对反应进行了优化。
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